AR050692A1 - Derivados de triazolopiridinilsulfanilo como inhibidores de quinasa map p38; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por tnf o por p38 - Google Patents
Derivados de triazolopiridinilsulfanilo como inhibidores de quinasa map p38; composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por tnf o por p38Info
- Publication number
- AR050692A1 AR050692A1 ARP050103357A ARP050103357A AR050692A1 AR 050692 A1 AR050692 A1 AR 050692A1 AR P050103357 A ARP050103357 A AR P050103357A AR P050103357 A ARP050103357 A AR P050103357A AR 050692 A1 AR050692 A1 AR 050692A1
- Authority
- AR
- Argentina
- Prior art keywords
- independently selected
- optionally substituted
- halo
- substituents independently
- conr5r6
- Prior art date
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 5
- 201000010099 disease Diseases 0.000 title abstract 3
- 230000001404 mediated effect Effects 0.000 title abstract 3
- 239000012826 P38 inhibitor Substances 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000001424 substituent group Chemical group 0.000 abstract 13
- 125000005843 halogen group Chemical group 0.000 abstract 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000004452 carbocyclyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 125000002950 monocyclic group Chemical group 0.000 abstract 4
- 125000001624 naphthyl group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- -1 NR5R6 Chemical group 0.000 abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 125000002757 morpholinyl group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000004193 piperazinyl group Chemical group 0.000 abstract 2
- 125000003386 piperidinyl group Chemical group 0.000 abstract 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- DBTDEFJAFBUGPP-UHFFFAOYSA-N Methanethial Chemical compound S=C DBTDEFJAFBUGPP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000000172 allergic effect Effects 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 208000010668 atopic eczema Diseases 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000005844 heterocyclyloxy group Chemical group 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 230000000414 obstructive effect Effects 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 210000002345 respiratory system Anatomy 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- Psychology (AREA)
Abstract
Uso de este compuesto en el tratamiento de una enfermedad, trastorno o afeccion mediada por TNF, o una enfermedad, trastorno o afeccion mediada por p38, en particular las enfermedades alérgicas y no alérgicas de las vías respiratorias, más particularmente enfermedades obstructivas o inflamatorias de las vías respiratorias, preferiblemente la enfermedad pulmonar obstructiva cronica. Reivindicacion 1: Un compuesto de formula (1), o una sal y/o solvato (incluyendo hidrato) farmacéuticamente aceptable del mismo, en la que: R1 es CH3, S(O)pCH3, S(O)pCH2CH3, CH2CH3, H o CH2S(O)pCH3; R1a es CH3 o CH2CH3, donde cada uno CH3 y CH2CH3 está opcionalmente sustituido con uno o más sustituyentes hidroxi; R2 es heteroarilo, heterociclilo, arilo, o carbociclilo; R3 es heteroarilo, heterociclilo, arilo, carbociclilo o R7; R7 es alquilo C1-6 (opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre OH, halo, NR5R6, alcoxi C1-6, - S(O)palquiloC1-6, CO2H, CONR5R6, heteroarilo, heterociclilo, arilo, carbociclilo, ariloxi, carbocicliloxi, heteroariloxi y heterocicliloxi); p es 0, 1 o 2; cada uno de R5 y R6 se selecciona independientemente entre H y alquilo C1-4, estando dicho alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre OH y halo; o R5 y R6, junto con el nitrogeno al que están unidos forman un grupo piperazinilo, piperidinilo, morfolinilo o pirrolidinilo, (estando cada uno de dichos piperazinilo, piperidinilo, morfolinilo y pirrolidinilo opcionalmente sustituido con uno o más OH); cada ôariloö significa independientemente fenilo o naftilo, estando dicho fenilo o naftilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -CN, -CO2H, OH, CONR5R6, NR5R6, R8 y R9; cada R8 se selecciona independientemente entre alquilo C1-6, alcoxi C1-6, -CO2alquiloC1-6, -S(O)alquiloC1-6, -COalquiloC1-6 y cicloaquilo C3-7; cada R8 está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre: alcoxi C1-6 (opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre OH, halo, CO2H, CONR5R6 y NR5R6); S(O)palquiloC1-6 (opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre OH, halo, CO2H, CONR5R6 y NR5R6); OH; halo; NR5R6; CO2H; CONR5R6; y R9; R9 es heteroarilo2, heterociclilo2, arilo2, carbociclilo2, aril2oxi, carbociclilo2oxi, heteroaril2oxi o heterociclil2oxi; ôarilo2ö significa fenilo o naftilo, estando dicho fenilo o naftilo opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -CN, -CO2H, OH, NR5R6 y CONR5R6; ôcarbocicliloö significa un sistema de anillo mono o bicíclico, saturado o parcialmente insaturado C3-10 en el anillo, opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -CN, -CO2H, OH, NR5R6, CONR5R6, R8 y R9; ôcarbociclilo2ö significa un sistema de anillo mono o bicíclico, saturado o parcialmente insaturado C3-10 en el anillo, opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre halo, -CN, - CO2H, NR5R6, OH y CONR5R6; cada ôheterocicliloö, y ôheterociclilo2ö, independientemente, significa un grupo mono o bicíclico saturado o parcialmente insaturado de 3 a 10 miembros que comprende de 1 a 4 heteroátomos en el anillo seleccionados independientemente entre N, O, y S; cada ôheteroariloö y cada ôheteroarilo2ö, independientemente, significa un grupo aromático mono o bicíclico de 5 a 10 miembros que comprende de 1 a 4 heteroátomos en el anillo seleccionados independientemente entre N, O y S (donde el numero total de átomos de S en el anillo no excede de 1, y el numero total de átomos de O en el anillo no excede de 1); cada grupo ôheterocicliloö y cada grupo ôheteroariloö está, independientemente, opcionalmente sustituido en uno o más átomos de carbono en el anillo con uno o más sustituyentes seleccionados independientemente entre halo, -CN, -CO2H, OH, NR5R6, CONR5R6, R8 y R9, y opcionalmente sustituido en uno o más átomos de nitrogeno en el anillo con uno o más sustituyentes seleccionados independientemente entre H y alquilo C1-6; y cada grupo ôheterociclilo2ö y cada grupo ôheteroarilo2ö está, independientemente, opcionalmente sustituido en uno o más átomos de carbono en el anillo con uno o más sustituyentes seleccionados independientemente entre halo, -CN, -CO2H, NR5R6, OH y CONR5R6, y opcionalmente sustituido en uno o más átomos de nitrogeno en el anillo con uno o más sustituyentes seleccionados independientemente entre H y alquilo C1- 6.
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| GB0418015A GB0418015D0 (en) | 2004-08-12 | 2004-08-12 | New compounds |
| US69155905P | 2005-06-17 | 2005-06-17 |
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